Catalog Number: 1363
Chemical Name: (2-Amino-4,5-dimethyl-3-thienyl)-[3-(trifluoromethyl)phenyl]methanone
Biological Activity
Allosteric potentiator at the adenosine A1 receptor; acts via agonist-dependent and -independent mechanisms. Enhances agonist affinity for, and increased t½ of dissociation from, the receptor. Also inhibits basal and forskolin-stimulated adenylyl cyclase (AC) activity in A1 receptors expressed in CHO cells, possibly via direct potentiation of constitutive receptor activity or by direct inhibition of AC. Active in vivo.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in ethanol and to 100 mM in DMSO
  • Purity:
  • Storage:
    Store at RT
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Structure-activity relationships for enhancement of adenosine A1 receptor binding by 2-amino-3-benzoylthiophenes.
    Bruns et al.
    Mol.Pharmacol., 1990;38:950
  2. Agonist-independent effect of an allosteric enhancer of the A1 adenosine receptor in CHO cells stably expressing the recombinant human A1 receptor.
    Kollias-Baker et al.
    J.Pharmacol.Exp.Ther., 1997;281:761
  3. PD 81,723, an allosteric enhancer of the A1 adenosine receptor, lowers the threshold for ischemic preconditioning in dogs.
    Mizumura et al.
    Circ.Res., 1996;79:415
  4. Adenosine A1 receptor-dependent and -independent effects of the allosteric enhancer PD 81,723.
    Musser et al.
    J.Pharmacol.Exp.Ther., 1999;288:446
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